P-糖蛋白介导的药代动力学及其药物相互作用

Effects of P-glycoprotein on the pharmacokinetics and interaction mediated by P-glycoprotein

P-糖蛋白是一个能量依赖性转运蛋白,能将许多结构不同的化合物逆向转运出细胞。它除了在肿瘤组织过度表达引起多药耐药外,在人体正常组织肝、肾、小肠、血脑屏障、肌肉组织、肾上腺等部位也有分布,对许多种药物的药代动力学具有调控作用。本文综述P-糖蛋白对药代动力学的作用及由P-糖蛋白的诱导和抑制所引起的药物相互作用。

P-glycoprotein is an ATP-driven efflux pump which transport a wide variety of structurally diverse compounds from the cell interior into the extracellular space. Apart from in tumor causing multidrug resistance, it is also localized in healthy tissues such as liver, kidney, intestinal, blood-brain barrier, muscles and adrenal gland etc, and can modulate the pharmacokinetics of a lot of compounds. The role of P-glycoprotein in absorption, distribution, metabolism, excretion and the drug-drug interaction mediated by induction and inhibition of P-glycoprotein are reviewed in this paper.